haspin kinase

Haspin-IN-3 is a potent haspin inhibitor with an IC50 of 14 nM.Haspin-IN-3 has anticancer activity.

MU1920 is an ATP-competitive, selective inhibitor of haspin with an IC50 of 6 nM. In mouse plasma and microsomes, it demonstrates favorable pharmacokinetic properties and metabolic stability. Although it lacks significant anticancer activity, MU1920 is suitable for developing chemical probes.

AZ1495 is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Which Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL).

LDN-192960 is a potent inhibitor of Haspin and DYRK2 (IC50s: 10 nM and 48 nM).

LDN-192960 hydrochloride is an inhibitor of Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) and Haspin, with IC50 values of 48 nM and 10 nM, respectively.

LDN-209929 2HCl is a potent and selective inhibitor of haspin kinase.

Haspin-IN-1 (compound 2a) is an inhibitor of haspin (haploid germ cell-specific nuclear protein kinase) with an IC50 of 119 nM. It also inhibits CLK1, DYRK1A, and CDK9 with IC50 values of 221 nM, 916.3 nM, and 406.8 nM, respectively. Haspin-IN-1 has potential for developing new anticancer drugs [1].

LDN-209929 dihydrochloride is a potent and selective inhibitor of haspin kinase (IC50= 55 nM), demonstrating 180-fold selectivity versus DYRK2 (IC50= 9.9 μM).

MELK-8a (NVS-MELK8a) is a potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), with an IC50 of 2 nM and an IC50 of 0.42 μM in cellular assays. MELK is crucial in regulating mitosis in cancer cells.

5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

CHR-6494 TFA is a potent haspin inhibitor with an IC50 of 2 nM, inhibiting histone H3T3 phosphorylation. It induces apoptosis in cancer cells, including melanoma and breast cancer, and is useful for cancer research.